AN IMPROVED METHOD FOR THE PREPARATION OF PHLOROGLUCINOL FROM 1,3,5-TRINITROBENZENE

Статья посвящена способу получения флороглюцина, представляющего интерес в качестве основы для конструирования лекарственных средств, полимеров различного назначения и малочувствительного взрывчатого вещества 1,3,5-триамино-2,4,6-тринитробензола. Современным и наиболее экологичным методом получения флороглюцина является каталитическое гидрирование 1,3,5-тринитробензола на палладиевом катализаторе до 1,3,5-триаминобензола и его последующий гидролиз. Использование палладиевых катализаторов позволяет проводить восстановление в мягких условиях, но их высокая стоимость обуславливает потребность в поиске путей снижения расхода палладия и, соответственно, себестоимости процесса. В данном исследовании показано, что использование 1 %-го Pd/сибунит (50 % к массе субстрата) в сочетании с водно-ацетоновым раствором в качестве среды при проведении гидрирования способствует более длительному сохранению активности катализатора. Установлено, что оптимальное соотношение ацетона и воды находится в диапазоне от 4:1 до 7:1. В этом случае может быть проведено до 20 циклов гидрирования без добавления свежего катализатора, за счет чего удается снизить расход палладия в три раза по сравнению с другими известными методиками. Кроме того, подход позволяет исключить из схемы синтеза токсичный растворитель метанол. Триаминобензол, полученный в ходе гидрирования, без выделения подвергается гидролизу в присутствии серной кислоты с образованием флороглюцина. Изучена зависимость выхода флороглюцина от мольного соотношения серной кислоты и тринитробензола. Установлено, что оптимальное соотношение серная кислота : тринитробензол составляет 2,0-2,4 моль/моль. Суммарный выход флороглюцина составляет 76 % в пересчете на тринитробензол. The study is concerned with a synthetic method for phloroglucinol that is of great concern as a scaffold for designing medicinal drugs, different-purpose polymers and the insensitive explosive 1,3,5-triamino-2,4,6-trinitrobenzene. The current and most eco-benign method for the synthesis of phloroglucinol is through catalytic hydrogenation of 1,3,5-trinitrobenzene over the Pd catalyst to 1,3,5-triaminobenzene followed by its hydrolysis. The use of Pd catalysts allows the reduction under mild conditions, but their high cost necessitates the need to find ways how to spare the Pd usage and, consequently, the process cost. Here we demonstrated that the use of 1% Pd/Sibunite (50% to substrate weight) combined with a water-acetone solution as the medium in hydrogenation allows the catalyst to keep active longer. The optimum acetone-to-water ratio was found to be between 4:1 and 7:1. In this case, as many as 20 hydrogenation runs can be done without a fresh catalyst added whereby the Pd usage can be lowered threefold when compared to the other common methods in use. Besides, this approach allows the toxic solvent methanol to be expelled from the synthetic protocol. Triaminobenzene resulting from the hydrogenation without isolation undergoes hydrolysis in the presence of sulfuric acid to furnish phloroglucinol. The relationship between the phloroglucinol yield and the molar ratio of sulfuric acid and trinitrobenzene was also explored. The optimum sulfuric acid-to-trinitrobenzene ratio was found to be 2.0-2.4 mol/mol. The overall yield of phloroglucinol was 76% on a trinitrobenzene basis.

Moral Bioenhancement: Widespread Harm and Broad Cooperation

<p>A controversial issue in contemporary bioethics has emerged in recent years: moral bioenhancement (MB). Human bioenhancement in general has seen its share of controversy, but it is generally agreed that there is potential to improve human physical and mental capacities through biotechnological interventions such as medicinal drugs and genetic modification. The discussion has turned to whether biotechnological interventions could similarly improve human moral capacities. Ingmar Persson and Julian Savulescu have argued that MB is imperative if humans are to survive into the future, because our current moral capacities do not equip us to address future catastrophic problems, Ultimate Harm, which will be caused by modern advanced scientific progress. I suggest related but distinct reasons why MB is appealing: scientific progress and deficient human moral capacities are jointly responsible for enormous amounts of harm all over the world, Widespread Harm, and MB has the potential to reduce that harm. Human moral capacities are deficient because of their dependence on what I call ‘moral intuitions’; evolved psychological traits that shape our many societies’ varied moral values, resulting in moral disagreement and the disruption of inter-group cooperation. Addressing modern problems requires a broader level of cooperation that is unlikely to be achieved by depending on our current moral intuitions. This is why our moral capacities should be improved. However, typical accounts of MB do not describe interventions that will improve our moral capacities in this way. They are focused on the vague objective of ‘making people morally better’, assuming that this will address human moral deficiency and that this will in turn address the resulting problems. ‘Making people morally better’ means making them more satisfactory to our current moral intuitions, which are the root of moral deficiency, so these MB strategies are unlikely to be effective. An alternative MB strategy, which I propose, instead focuses on the objective of modifying current moral intuitions so that they promote broad cooperation. This will result in improved moral capacities in the sense that our moral capacities will be more practically useful to us. However, because this strategy disregards the importance of satisfying our current moral intuitions, it will be morally unpalatable. This is its main disadvantage over the typical MB strategy, though it is better at handling many common objections. Ultimately, there are a number of practical concerns that cannot be completely satisfactorily responded to even by my new MB strategy, such as the issues of mandatory MB and of fine-tuning our moral capacities. These concerns may mean that MB is too risky, and therefore not the best course of action in response to modern problems rooted in scientific progress and moral deficiency, particularly since we have promising alternatives available such as traditional moral enhancement techniques and further scientific progress. The prospect of MB should continue to be investigated, but it should focus on improving upon our current problematic moral intuitions rather than better satisfying them.</p>

Moral Bioenhancement: Widespread Harm and Broad Cooperation

<p>A controversial issue in contemporary bioethics has emerged in recent years: moral bioenhancement (MB). Human bioenhancement in general has seen its share of controversy, but it is generally agreed that there is potential to improve human physical and mental capacities through biotechnological interventions such as medicinal drugs and genetic modification. The discussion has turned to whether biotechnological interventions could similarly improve human moral capacities. Ingmar Persson and Julian Savulescu have argued that MB is imperative if humans are to survive into the future, because our current moral capacities do not equip us to address future catastrophic problems, Ultimate Harm, which will be caused by modern advanced scientific progress. I suggest related but distinct reasons why MB is appealing: scientific progress and deficient human moral capacities are jointly responsible for enormous amounts of harm all over the world, Widespread Harm, and MB has the potential to reduce that harm. Human moral capacities are deficient because of their dependence on what I call ‘moral intuitions’; evolved psychological traits that shape our many societies’ varied moral values, resulting in moral disagreement and the disruption of inter-group cooperation. Addressing modern problems requires a broader level of cooperation that is unlikely to be achieved by depending on our current moral intuitions. This is why our moral capacities should be improved. However, typical accounts of MB do not describe interventions that will improve our moral capacities in this way. They are focused on the vague objective of ‘making people morally better’, assuming that this will address human moral deficiency and that this will in turn address the resulting problems. ‘Making people morally better’ means making them more satisfactory to our current moral intuitions, which are the root of moral deficiency, so these MB strategies are unlikely to be effective. An alternative MB strategy, which I propose, instead focuses on the objective of modifying current moral intuitions so that they promote broad cooperation. This will result in improved moral capacities in the sense that our moral capacities will be more practically useful to us. However, because this strategy disregards the importance of satisfying our current moral intuitions, it will be morally unpalatable. This is its main disadvantage over the typical MB strategy, though it is better at handling many common objections. Ultimately, there are a number of practical concerns that cannot be completely satisfactorily responded to even by my new MB strategy, such as the issues of mandatory MB and of fine-tuning our moral capacities. These concerns may mean that MB is too risky, and therefore not the best course of action in response to modern problems rooted in scientific progress and moral deficiency, particularly since we have promising alternatives available such as traditional moral enhancement techniques and further scientific progress. The prospect of MB should continue to be investigated, but it should focus on improving upon our current problematic moral intuitions rather than better satisfying them.</p>

Multimorbidity, psychoactive substance use and psychological distress among acute medically ill patients: a cross-sectional study

BackgroundIn order to target the complex health needs of patients with multimorbidity using psychoactive substances, knowledge regarding the association between substance use and multimorbidity in an acute setting is needed.AimsExamine psychoactive substance use patterns among acute medically ill patients, and determine the association between multimorbidity and substance use, and psychological distress.DesignCross-sectional study.Setting and participants2874 acute medically ill patients admitted to a medical emergency department in Oslo, Norway.MeasurementsPrimary outcome: multimorbidity recorded by the presence of ≥2 International Classification of Diseases 10th revision—physical and/or mental health conditions per patient, extracted from medical records. Predictor variables: self-reported data on age, sex, occupational status, psychological distress (Hopkins Symptom Check List-5), alcohol use (Alcohol Use Disorder Identification Test-4) and results from blood samples on psychoactive medicinal and illicit drugs.FindingsOf all patients, 57.2% had multimorbidity. Of these, 62.6% reported psychological distress, 85.5% consumed either alcohol, medicinal and/or illicit drugs and 64.4% combined alcohol with psychoactive medicinal drugs. Patients with risky alcohol use were more likely to have multimorbidity compared with patients with low-risk alcohol use (OR 1.53; 95% CI 1.05 to 2.24). Patients using psychoactive medicinal drugs were more likely to have multimorbidity compared with non-users (OR 1.34; 95% CI 1.07 to 1.67).ConclusionMultimorbidity was associated with psychoactive medicinal drug and risky alcohol use, and psychological distress. Substance use was widespread, with alcohol and psychoactive medicinal drugs most frequently combined. Monitoring substance use among multimorbid patients is necessary to develop tailored treatments, and reduce burden on the healthcare system.

A Conceptual Study of Upanaha Swedana

Swedana Karma is undertaken by inducing sweating from the application of heat. There are many methods used to achieve this, with Upanaha Swedana being one of them. Upanaha Swedana is a standard treatment modality used in Ayurveda for the management of pain and inflammation. It is a localized treatment wherein a combination of medicinal drugs are prepared, made into a poultice, heated and applied at the affected site. This is meant to reduce the local inflammation and act as a topical analgesic. The procedure is divided into three phases which are: Purva Karma (pre-therapy procedures), the preparation of the Upanaha Swedana material is done, Pradhana Karma (main therapeutic procedures) the prepared Upanaha Swedana material is applied to the patient and Paschat Karma (post-therapy procedures) after waiting the specified times, the Upahana Swedana is removed following proper procedures. The present conceptual study was done based on the need of the day to elaborate the process of conducting Upanaha Swedana. For this, various Ayurvedic texts, digital libraries referencing Samhita were searched and the following headings were selected, types of data, types of reports and functionalities. This article seeks to explore this treatment modality and outline the general approach to be followed while conducting the procedure of Upanaha Swedana.

High-performance thin layer chromatography: A powerful analytical technique in pharmaceutical drug discovery

HPTLC is an advanced type of planar chromatography used extensively in the recent years for fingerprinting of medicinal plants, products and for screening lichen substances, quantification of active ingredients and herbal drugs, phytochemical and biomedical analysis and also used to check of presence of adulterants in the formulation. It is more sensitive and possible to run more sample in a short period of time, by using small amount of solvent. It is one of the sophisticated instrumental techniques based on the full capabilities of thin layer chromatography. In this paper, a brief discussion of the type of instrument used in HPTLC, its entire approach, and how this procedure is superior to TLC is presented. This article attempts to concentrate on the use of HPTLC by including examples of medications, medicinal drugs, and formulations that have been analyzed using HPTLC.